Cationic stearylamine-containing biodegradable microparticles for DNA delivery

Technical aspects for preparing a new type of cationic stearylamine (SA)-containing microparticle as a potential drug delivery system for negatively charged therapeutics were investigated. Cationic biodegradable microparticles based on poly(lactide) and poly(lactide-co-glycolide) were prepared upon...

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Bibliographic Details
Published in:Journal of microencapsulation 2004-02, Vol.21 (1), p.25-36
Main Authors: Kusonwiriyawong, C., Atuah, K., Alpar, O. H., Merkle, H. P., Walter, E.
Format: Article
Language:English
Subjects:
Amines - chemistry
Biocompatible Materials - chemistry
Biological and medical sciences
Cationic biodegradable microparticles
DNA
DNA - administration & dosage
Drug Carriers - chemistry
Drug Delivery Systems - methods
Feasibility Studies
General pharmacology
Humans
Medical sciences
Microspheres
Particle Size
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
poly(lactide)
poly(lactide-co-glycolide)
solvent evaporation
Solvents - chemistry
spray-drying
stearylamine
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Summary:Technical aspects for preparing a new type of cationic stearylamine (SA)-containing microparticle as a potential drug delivery system for negatively charged therapeutics were investigated. Cationic biodegradable microparticles based on poly(lactide) and poly(lactide-co-glycolide) were prepared upon incorporation of SA either by solvent evaporation or by spray-drying. Water-insoluble SA offers the advantage over other water-soluble cationic compounds that it can be dissolved directly in the organic solution together with the polymers. This facilitated the subsequent preparation of the microparticle formulations. Particle size was controlled by the respective process parameters, resulting in either large polymer aggregates within the range 50-100 µm or small spherical microparticles within the range 1-10 µm. The incorporation of SA into the formulations also improved particle characteristics in terms of re-dispersibility, reduced sticking, and particle size uniformity. Both circular plasmid DNA (5 kbp) and linear salmon DNA (0.5 kbp) were efficiently adsorbed to the cationic SA microparticle surfaces. Preliminary tests on the release of DNA from spray-dried SA microparticles showed an immediate burst release, which was followed by a delayed second release phase for more than 4 weeks. The cationic SA microparticles might provide a potential drug-delivery system to improve the efficacy for protein and DNA-type therapeutics.
ISSN:0265-2048
1464-5246
DOI:10.1080/02652040410001653777